US5061492A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Prolonged release microcapsule of a water-soluble drug
Assignee: Takeda Pharmaceutical Co Ltd
•
Filing: 1990-01-24
•
Granted: 1991-10-29
•
Expires: 2010-01-24
Abstract
Abstract A microcapsule produced by preparing a water-in-oil emulsion comprising an inner aqueous layer containing said water-soluble drug and a drug retaining substance therefor and an oil layer containing a polymer substance, then thickening or solidifying said inner aqueous layer to a viscosity of not lower than about 5000 centiposes and finally subjecting the resulting emulsion to in water drying gives prolonged release of water-soluble drug.
Inventors
- 👤 Hiroaki Okada
- 👤 Yasuaki Ogawa
- 👤 Takatsuka Yashiki
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-05 21:20
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/48; A61K9/50; A61K9/5005; A61K9/5021; A61K9/5031; A61K38/00; A61K38/04; A61K38/05; A61K38/08; A61K38/09; A61K38/16; A61K38/17; A61K38/33; A61K38/36; A61K38/37; A61K9/14; A61K9/16; A61K9/1605; A61K9/1629; A61K9/1641; A61K9/1647; A61K9/1682; A61K9/1694; A61K9/5089; B; B01; B01J; B01J13/00; B01J13/02; B01J13/06; B01J13/12; B01J13/125; Y; Y10; Y10S; Y10S424/00; Y10S424/15; Y10T; Y10T428/00; Y10T428/29; Y10T428/2982; Y10T428/2984; Y10T428/2985; Y10T428/2989
Claims Analysis
Total Claims: 9
Claim 1
Independent Claim
127 words
An injectable preparation comprising a therapeutically effective amount of spherical microcapsules and a pharmaceutically acceptable vehicle, wherein said spherical microcapsules have an average diameter of 2-200 μm, and comprise particles of a mixture of a water-soluble non-polypeptidic drug and a drug-retaining substance therefor selected from the group consisting of gelatin, albumin, pectin and agar, the weight ratio of the drug-retaining substance to the water-soluble non-polypeptidic drug being in the range of about 9/1 to about 0.3/1, the particles being dispersed in a spherical microcapsule matrix composed of a biodegradable polymer, said biodegradable polymer being a copolymer of lactic acid and glycolic acid having a comonomer ratio within the range of about 100/0 to 50/50 and an average molecular weight within the range of about 5,000 to 200,000.
Claim 2
Dependent Claim
127 words
An injectable preparation comprising a therapeutically effective amount of spherical microcapsules and a pharmaceutically acceptable vehicle, wherein said spherical microcapsules have an average diameter of 2-200 μm, and comprise particles of a mixture of a water-soluble non-polypeptidic drug and a drug-retaining substance therefor selected from the group consisting of gelatin, albumin, pectin and agar, the weight ratio of the drug-retaining substance to the water-soluble non-polypeptidic drug being in the range of about 9/1 to about 0.3/1, the particles being dispersed in a spherical microcapsule matrix composed of a biodegradable polymer, said biodegradable polymer being a copolymer of lactic acid and glycolic acid having a comonomer ratio within the range of about 100/0 to 50/50 and an average molecular weight within the range of about 5,000 to 200,000.
Claim 3
Dependent Claim
77 words
An injectable preparation as recited in claim 1, wherein the water-soluble non-polypeptidic drug is a member selected from the group consisting of an antibiotic, an antitumor agent, an antipyretic, an analgesic, an anti-inflammatory agent, an antitussive, an expectorant, a sedative, a muscle relaxant, an antiepileptic, an antiulcer agent, an antidepressant, an antiallergic drug, a cardiotonic, an antiarrhythmic agent, a vasodilator, an antihypertensive diuretic, an antidiabetic, an anticoagulant, a hemostatic, an antituberculotic, a hormone drug and an antinarcotic.
Claim 4
Dependent Claim
51 words
An injectable preparation as recited in claim 2, wherein the antitumor agent is selected from the group consisting of bleomycin hydrochloride, methotrexate, actinomycin D, mitomycin C, vinblastine sulfate, vincristine sulfate, daunorubicin hydrochloride, adriamycin, neocarcinostatin, cytosine arabinoside, fluorouracil, krestin, picibanil, lentinan, levamisole, bestatin, azimexon, glycyrrhizin, poly I:C, poly A:U and poly ICLC.
Claim 5
Dependent Claim
55 words
An injectable preparation as recited in claim 1, wherein the water-soluble non-polypeptidic drug is an antitumor agent selected from the group consisting of bleomycin hydrochloride, methotrexate, actinomycin D, mitomycin C, vinblastine sulfate, vincristine sulfate, daunorubicin hydrochloride, adriamycin, neocarcinostatin, cytosine arabinoside, fluorouracil, krestin, picibanil, lentinan, levamisole, bestatin, azimexon, glycyrrhizin, poly I:C, poly A:U and poly ICLC.
Claim 6
Dependent Claim
15 words
An injectable preparation as recited in claim 4, wherein the antitumor agent is mitomycin C.
Claim 7
Dependent Claim
39 words
An injectable preparation as recited in claim 1, wherein the water-soluble non-polypeptidic drug is a member selected from the group consisting of sodium salicylate, sulpyrine, sodium flufenamate, sodium diclofenac, sodium indomethacin, morphine hydrochloride, pethidine hydrochloride, levorphanol tartrate and oxymorphone.
Claim 8
Dependent Claim
28 words
An injectable preparation as recited in claim 1, wherein the water-soluble non-polypeptidic drug is a member selected from the group consisting of sulpyrine, morphine hydrochloride and sodium diclofenac.
Claim 9
Dependent Claim
24 words
An injectable preparation as recited in claim 1, wherein the comonomer ratio of the copolymer of lactic acid and glycolic acid is about 78/22.
References Cited (Backward Citations)
US3523906A
Cited
US3645911A
Cited
US3691090A
Cited
US3773919A
Cited
US4272398A
Cited
US4234571A
Cited
US4622244A
Cited
US4273920A
Cited
GB2088314A
Cited
FR2491351A1
Cited
EP0052510B1
Cited
US4675189A
Cited
EP0058481A1
Cited
US4637905A
Cited
US4652441A
Cited
US4711782A
Cited
US4917893A
Cited
US4849228A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1994-10-28 | 1995-04-29 | 1995-10-29 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1998-10-28 | 1999-04-29 | 1999-10-29 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2002-10-28 | 2003-04-29 | 2003-10-29 | $7700.00 | Window Closed / Lapsed |